Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
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β-N-Cyanoethyl Acyl Hydrazide Derivatives: A New Class of β-Glucuronidase Inhibitors
Khalid Mohammed KhanShahida ShujaatShagufta RahatSafdar HayatAtta-ur-RahmanMuhammad Iqbal Choudhary
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2002 Volume 50 Issue 11 Pages 1443-1446

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Abstract

Eight new β-N-substituted acyl hydrazides along with their corresponding acyl derivatives were synthesized and screened for in vitro β-glucuronidase inhibition and found to be active against the enzyme. All of these compounds were found to be noncompetitive inhibitors except for N′-(2-cyanoethyl)-4-hydroxy benzohydrazide (10), which was found to be an uncompetitive inhibitor. Structure–activity relationship studies indicated that the benzyloxy group present in compounds 12 and 13 is responsible for the β-glucuronidase inhibition activity.

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© 2002 The Pharmaceutical Society of Japan
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